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Namespace Prefixes

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Statements

Subject Item
n2:DB00998
rdf:type
n3:Drug
n3:description
Frovatriptan (Frova®) is a triptan drug developed by Vernalis for the treatment of migraine headaches, in particular those associated with menstruation. The product is licensed to Endo Pharmaceuticals in North America and Menarini in Europe.[1] Frovatriptan causes vasoconstriction of arteries and veins that supply blood to the head. It is available as 2.5 mg tablets. Frovatriptan has mean terminal elimination half-life of approximately 26 hours, which is substantially longer than other triptans. Frovatriptan is available only by prescription in the United States, where a secondary New Drug Approval (sNDA) was filed in July 2006[2] and which is currently pending.[3] The FDA anticipates completing its review of this application on or before the current PDUFA (Prescription Drug User Fee Act) review date of August 19, 2007. If the sNDA is approved, Frova® will be the only medication indicated in the U.S. for the short-term prevention of menstrual migraine (MM).
n3:dosage
n4:271B4CEE-363D-11E5-9242-09173F13E4C5 n4:271B4CEF-363D-11E5-9242-09173F13E4C5
n3:generalReferences
# Markus F, Mikko K: Frovatriptan review. Expert Opin Pharmacother. 2007 Dec;8(17):3029-33. "Pubmed":http://www.ncbi.nlm.nih.gov/pubmed/18001261 # Easthope SE, Goa KL: Frovatriptan. CNS Drugs. 2001;15(12):969-76; discussion 977-8. "Pubmed":http://www.ncbi.nlm.nih.gov/pubmed/11735616 # Balbisi EA: Frovatriptan: a review of pharmacology, pharmacokinetics and clinical potential in the treatment of menstrual migraine. Ther Clin Risk Manag. 2006 Sep;2(3):303-8. "Pubmed":http://www.ncbi.nlm.nih.gov/pubmed/18360605 # Balbisi EA: Frovatriptan succinate, a 5-HT1B/1D receptor agonist for migraine. Int J Clin Pract. 2004 Jul;58(7):695-705. "Pubmed":http://www.ncbi.nlm.nih.gov/pubmed/15311727 # Elkind AH, Wade A, Ishkanian G: Pharmacokinetics of frovatriptan in adolescent migraineurs. J Clin Pharmacol. 2004 Oct;44(10):1158-65. "Pubmed":http://www.ncbi.nlm.nih.gov/pubmed/15342617 # Jhee SS, Shiovitz T, Crawford AW, Cutler NR: Pharmacokinetics and pharmacodynamics of the triptan antimigraine agents: a comparative review. Clin Pharmacokinet. 2001;40(3):189-205. "Pubmed":http://www.ncbi.nlm.nih.gov/pubmed/11327198
n3:group
approved investigational
n3:halfLife
26 hours
n3:indication
For the acute treatment of migraine attacks with or without aura in adults.
n3:manufacturer
n27:271B4CEB-363D-11E5-9242-09173F13E4C5
owl:sameAs
n24:DB00998 n25:DB00998
dcterms:title
Frovatriptan
adms:identifier
n9:PA164754891 n11:Frovatriptan n12:70378 n13:DB00998 n14:50073689 n17:77992 n18:46506288 n19:63481-025-09
n3:mechanismOfAction
Three distinct pharmacological actions have been implicated in the antimigraine effect of the triptans: (1) stimulation of presynaptic 5-HT<sub>1D</sub> receptors, which serves to inhibit both dural vasodilation and inflammation; (2) direct inhibition of trigeminal nuclei cell excitability via 5-HT<sub>1B/1D</sub> receptor agonism in the brainstem and (3) vasoconstriction of meningeal, dural, cerebral or pial vessels as a result of vascular 5-HT<sub>1B</sub> receptor agonism.
n3:packager
n27:271B4CE9-363D-11E5-9242-09173F13E4C5 n27:271B4CEA-363D-11E5-9242-09173F13E4C5 n27:271B4CE7-363D-11E5-9242-09173F13E4C5 n27:271B4CE8-363D-11E5-9242-09173F13E4C5 n27:271B4CE5-363D-11E5-9242-09173F13E4C5 n27:271B4CE6-363D-11E5-9242-09173F13E4C5
n3:patent
n10:5464864 n10:5962501 n10:2113726 n10:2152630
n3:routeOfElimination
Radiolabeled compounds excreted in urine were unchanged frovatriptan, hydroxylated frovatriptan, N-acetyl desmethyl frovatriptan, hydroxylated N-acetyl desmethyl frovatriptan and desmethyl frovatriptan, together with several other minor metabolites. Less than 10% of frovatriptan was excreted in urine after an oral dose.
n3:synonym
Frovatriptan succinate Allergo filmtabletten
n3:toxicity
There is no direct experience of any patient taking an overdose of Frovatriptan. The maximum single dose of frovatriptan given to male and female patients with migraine was 40 mg (16 times the clinical dose) and the maximum single dose given to healthy male subjects was 100 mg (40 times the clinical dose) without significant adverse events.
n3:volumeOfDistribution
* 4.2 L/kg [males] * 3 L/kg [females]
n3:foodInteraction
Take without regard to meals. Food does not affect amount of absorption but delays maximal levels by about 1 hour.
n3:proteinBinding
Binding to serum proteins is low (approximately 15%). Reversible binding to blood cells at equilibrium is approximately 60%.
n3:synthesisReference
Samir Naik, Anthony Crasto, Narendra Joshi, Sachin Srivastava, "Amorphous frovatriptan succinate and process for the preparation thereof." U.S. Patent US20070299123, issued December 27, 2007.
n6:hasConcept
n7:M0281019
foaf:page
n21:frovatriptan.html n26:fro1622.shtml n28:frova.htm
n3:IUPAC-Name
n5:271B4CF4-363D-11E5-9242-09173F13E4C5
n3:InChI
n5:271B4CFA-363D-11E5-9242-09173F13E4C5
n3:Molecular-Formula
n5:271B4CF9-363D-11E5-9242-09173F13E4C5
n3:Molecular-Weight
n5:271B4CF6-363D-11E5-9242-09173F13E4C5
n3:Monoisotopic-Weight
n5:271B4CF7-363D-11E5-9242-09173F13E4C5
n3:SMILES
n5:271B4CF8-363D-11E5-9242-09173F13E4C5
n3:Water-Solubility
n5:271B4D0A-363D-11E5-9242-09173F13E4C5 n5:271B4CF2-363D-11E5-9242-09173F13E4C5
n3:logP
n5:271B4D0B-363D-11E5-9242-09173F13E4C5 n5:271B4CF3-363D-11E5-9242-09173F13E4C5 n5:271B4CF0-363D-11E5-9242-09173F13E4C5
n3:logS
n5:271B4CF1-363D-11E5-9242-09173F13E4C5
n15:hasATCCode
n16:N02CC07
n3:H-Bond-Acceptor-Count
n5:271B4D00-363D-11E5-9242-09173F13E4C5
n3:H-Bond-Donor-Count
n5:271B4D01-363D-11E5-9242-09173F13E4C5
n3:InChIKey
n5:271B4CFB-363D-11E5-9242-09173F13E4C5
n3:Polar-Surface-Area--PSA-
n5:271B4CFC-363D-11E5-9242-09173F13E4C5
n3:Polarizability
n5:271B4CFE-363D-11E5-9242-09173F13E4C5
n3:Refractivity
n5:271B4CFD-363D-11E5-9242-09173F13E4C5
n3:Rotatable-Bond-Count
n5:271B4CFF-363D-11E5-9242-09173F13E4C5
n3:absorption
Frovatriptan is rapidly absorbed from the duodenum, but has low oral bioavailability.
n3:affectedOrganism
Humans and other mammals
n3:casRegistryNumber
158747-02-5
n3:category
n3:clearance
* 220 mL/min [male receiving IV dose of 0.8 mg] * 130 mL/min [Female receiving IV dose of 0.8 mg]
n3:containedIn
n22:271B4CED-363D-11E5-9242-09173F13E4C5 n22:271B4CEC-363D-11E5-9242-09173F13E4C5
n3:Bioavailability
n5:271B4D06-363D-11E5-9242-09173F13E4C5
n3:Ghose-Filter
n5:271B4D08-363D-11E5-9242-09173F13E4C5
n3:MDDR-Like-Rule
n5:271B4D09-363D-11E5-9242-09173F13E4C5
n3:Number-of-Rings
n5:271B4D05-363D-11E5-9242-09173F13E4C5
n3:Physiological-Charge
n5:271B4D04-363D-11E5-9242-09173F13E4C5
n3:Rule-of-Five
n5:271B4D07-363D-11E5-9242-09173F13E4C5
n3:Traditional-IUPAC-Name
n5:271B4CF5-363D-11E5-9242-09173F13E4C5
n3:pKa--strongest-acidic-
n5:271B4D02-363D-11E5-9242-09173F13E4C5
n3:pKa--strongest-basic-
n5:271B4D03-363D-11E5-9242-09173F13E4C5